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Pregabalin controlled release preparation, and preparation method thereof

A technology of pregabalin and controlled-release preparations, which is applied in the field of pregabalin controlled-release preparations for the treatment of neuropathic pain and its preparation, which can solve the problems of loss of curative effect, failure to reproduce multi-dose drug bioavailability, malabsorption, etc. , to achieve the effect of prolonging the residence time, prolonging the drug action time, and reducing the number of medications

Inactive Publication Date: 2014-02-19
HANGZHOU SHARPLY PHARM R&D INSTIT +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the release of the drug from the system is well controlled, due to the effect of gastric emptying, it takes about 3 hours to reach the rectum, resulting in most of the drug being released at a non-optimal site, making the sustained release formulation unable to reproduce the effect of multiple doses. bioavailability
[0013] Pregabalin is absorbed in the gastrointestinal tract. Pharmacokinetic studies have shown that the absorption of pregabalin from the small intestine to the large intestine increases, while the absorption of pregabalin is less in the hepatic flexure of the colon. For traditional slow-release preparations, it is transferred to the hepatic flexure of the colon in about 6 hours. It is poorly absorbed and loses its efficacy in the rest of the gut

Method used

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  • Pregabalin controlled release preparation, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: Prepare 1000 pregabalin controlled-release preparations and adopt the following prescription:

[0036] Pregabalin 330g

[0037] Calcium hydrogen phosphate 103.5g

[0038] Carbomer 30g

[0039] Polycarbophil 30g

[0040] Hypromellose 3cp 30g

[0041] Sodium bicarbonate 60g

[0042] Magnesium Stearate 15g

[0043] Micronized silica gel 1.5g

[0044] Its preparation method:

[0045] 1. Pass pregabalin pretreatment through an 80-mesh sieve, calcium hydrogen phosphate pass through an 80-mesh sieve, and sodium bicarbonate, magnesium stearate, and micropowder silica gel pass through an 80-mesh sieve respectively;

[0046] 2. Prepare 5% hydroxypropyl methylcellulose and 75% ethanol solution as a binder;

[0047] 3. Mix pregabalin, calcium hydrogen phosphate, carbomer, and polycarbophil, and use 5% hypromellose 75% ethanol solution to granulate;

[0048] 4. Granulate after drying the wet granules;

[0049] 5. Mix the granulated granules with additional auxi...

Embodiment 2

[0052] Embodiment 2: prepare 1000 pregabalin controlled-release tablets, adopt following prescription:

[0053] Pregabalin 330g

[0054] Microcrystalline Cellulose 102 123.5g

[0055] Carbomer 70g

[0056] Hypromellose 3cp 20g

[0057] Octadecanol 45g

[0058] Magnesium Stearate 10g

[0059] Micronized silica gel 1.5g

[0060] Preparation method: 1. Pretreatment pregabalin is passed through an 80-mesh sieve, and stearyl alcohol, magnesium stearate, and micropowdered silica gel are respectively passed through an 80-mesh sieve;

[0061] 2. Pregabalin, microcrystalline cellulose, carbomer, hypromellose, stearyl alcohol. Micropowder silica gel is mixed, then mixed evenly with magnesium stearate;

[0062] 3. Perform direct compression according to the test results of the intermediate content to obtain pregabalin sustained-release tablets.

Embodiment 3

[0063] Embodiment 3: prepare 1000 pregabalin controlled-release tablets, adopt following prescription:

[0064] Pregabalin 330g

[0065] Lactose 87g

[0066] Sodium Alginate 80g

[0067] Calcium chloride 40g

[0068] Polycarbophil 6g

[0069] Octadecanol 45g

[0070] Micronized silica gel 12g

[0071] Makes 1000 capsules

[0072] Its preparation method:

[0073] 1. Pass pregabalin pretreatment through an 80-mesh sieve, and lactose, stearyl alcohol, and micropowdered silica gel respectively pass through an 80-mesh sieve;

[0074] 2. Mix pregabalin, lactose, polycarbophil, sodium alginate, calcium chloride, stearyl alcohol, and micronized silica gel evenly;

[0075] 3. Perform direct compression according to the test results of the intermediate content to obtain pregabalin sustained-release tablets.

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Abstract

The invention relates to a pregabalin controlled release preparation, and a preparation method thereof. The pregabalin controlled release preparation comprises following ingredients, by weight, 30 to 75% of pregabalin, 5 to 40% of a filling material, 5 to 30% of a sustained-release material, 1 to 10% of an adhesive, and the balance an auxiliary material. The auxiliary material is one or more selected from magnesium stearate, talc, superfine silica powder, cetanol, octadecanol, liquid paraffin, stearic acid, sodium bicarbonate, magnesium carbonate and calcium carbonate; the sustained-release material is one or a mixture of more selected from ethyl cellulose, carbomer, polycarbophil, alginate, hydroxypropyl methyl cellulose, polyacrylic resin, and carnauba wax. The pregabalin controlled release preparation is capable of prolonging residence time of medicine in stomach, releasing long-lasting release and absorption of medicine, and further increasing bioavailability of medicine.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a drug pregabalin controlled-release preparation for treating neuropathic pain and a preparation method thereof. Background technique [0002] Pain is an unpleasant sensory and emotional experience described by or in terms of tissue damage. Pain can be divided into acute and chronic pain according to the course of the disease, and can also be divided into nociceptive pain, neuropathic pain and mixed pain according to the pathophysiology. Among them, neuropathic pain is pain caused by damage, disease or dysfunction of the peripheral or central nervous system, which can be divided into central and peripheral neuropathic pain, metabolic abnormalities, trauma, ischemia, poisoning, genetic factors, infection, Compression, immune abnormalities and other reasons can be caused. Multiple mechanisms can lead to central and peripheral neuropathic pain. Peripheral mechanisms inc...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/22A61K9/52A61K31/197A61K47/04A61P29/00A61P25/02A61P25/08
Inventor 范敏华姜新东刘华
Owner HANGZHOU SHARPLY PHARM R&D INSTIT
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